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/ 组胺受体 / Tripelennamine HCl

盐酸吡苄明 /Tripelennamine HCl {[allProObj[0].p_purity_real_show]}

货号：A147384 同义名： 去敏灵;盐酸曲吡那敏 / Pyribenzamine HCl;Tripelennamine hydrochloride

Tripelennamine HCl is an antagonist of H1-receptor that used as a psychoactive drug with antipruritic activity.

Tripelennamine HCl 化学结构 CAS号：154-69-8
Tripelennamine HCl 化学结构
CAS号：154-69-8
Tripelennamine HCl 3D分子结构
CAS号：154-69-8
Tripelennamine HCl 化学结构 CAS号：154-69-8
Tripelennamine HCl 3D分子结构 CAS号：154-69-8
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Tripelennamine HCl 纯度/质量文件 产品仅供科研

货号：A147384 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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产品名称 H1 receptor ↓ H2 receptor ↓ H3 receptor ↓ H4 receptor ↓ Histamine receptor ↓ 其他靶点 纯度
Hydroxyzine 2HCl 99+%
Cyclizine ✔ 97%
Loratadine +

B(0)AT2, IC50: 4 μM

 		98%
Desloratadine ++

Histamine H1 receptor, IC50: 51 nM

 		98%
Doxylamine succinate ✔ 99%
Ebastine ✔ 98%
Tripelennamine HCl +

H1 receptor, IC50: 30 μM

 		98%
Meclizine dihydrochloride ✔ 98%
Chlorpheniramine maleate +++

Histamine H1 receptor, IC50: 12 nM

 		99%
Diphenhydramine HCl ✔ 99%
Alcaftadine ++++

H1 receptor, pKi: 8.5

 		++

H2 receptor, pKi: 7.2

 		99%+
Fexofenadine HCl ++

Histamine H1 receptor, IC50: 246 nM

 		99%+
Bilastine +++

H1 receptor, Ki: 44.15 nM

 		98%
Pemirolast potassium ✔ 98%
Bepotastine besilate +

Histamine H1 receptor, pIC50: 5.7

 		98%
Mizolastine +++

Histamine H1 receptor, IC50: 47 nM

 		98%
Brompheniramine maleate ✔ 98%
Carbinoxamine maleate salt ✔ 99+%
Clemastine fumarate ++++

Histamine H1 receptor, IC50: 3 nM

 		98%
Ketotifen fumarate salt ✔ 95%
Rupatadine Fumarate ++

Histamine H1 receptor, Ki: 102 nM

 		PAFR 98%
Famotidine ✔ 97%
Roxatidine Acetate HCl +

Histamine H2 receptor, IC50: 3.2 μM

 		98%
Lafutidine ✔ 99%
Cimetidine ✔ 98%
Nizatidine ++++

Histamine H2 receptor, IC50: 0.9 nM

 		AChE 98%
Ranitidine ✔ 99%
Betahistine +

Histamine H3 receptor, IC50: 1.9 μM

 		98%
Ciproxifan maleate +++

Histamine H3 receptor, IC50: 9.2 nM

 		99%+
S 38093 ++

rat H3 receptor, Ki: 1.44 μM

human H3 receptor, Ki: 1.2 μM

 		98%
JNJ-7777120 ++++

Histamine H4 receptor, Ki: 4.5 nM

 		98%
Azelastine HCl ✔ 98%
Epinastine HCl ✔ 98%
Levodropropizine ✔ 97%
Cyproheptadine hydrochloride ✔ 98%
Hesperetin ✔ 97%
Olopatadine HCl ✔ 98%
Mianserin hydrochloride ✔ 99+%
Buclizine 2HCl ✔ 97%
Latrepirdine 2HCl ✔ GluR 98%
Cetirizine 2HCl ✔ 98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Tripelennamine HCl 生物活性

靶点

  • H1 receptor

    H1 receptor, IC50:30 μM
描述 Tripelennamine (Hydrochloride) is a widely used H1 antagonist, inhibiting PhIP (glucuronidation of 2-amino-1-methyl-6-phenylimidazo[4,5-b] pyridine) glucuronidation with IC50 of 30 μM[3]. Tripelennamine (0.3-10.0 mg/kg) produced only saline-appropriate responding and dose-related decreases in response rates. Tripelennamine does not enhance the morphine-like discriminative stimulus properties of pentazocine in the pigeon, as it does in the rat[4]. Tripelennamine (10 and 20 mg/kg i.p.) showed some antinociceptive activity, which was not antagonized by naloxone. Pentazocine antinociception was potentiated by simultaneous administration of a large dose (20 mg/kg) but not a small dose (5 mg/kg) of tripelennamine. The effect of tripelennamine on pentazocine antinociception is additive; very little was through a mechanism of inhibition of pentazocine metabolism[5]. Tripelennamine (1.25 mg/kg, IV) produced antinociception, mydriasis and tachycardia without affecting behavior[6].

Tripelennamine HCl 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00316381 Myocardial Infarction Not Applicable Completed - Poland ... 展开 >> III Division of Cardiology Silesian School of Medicine Katowice, Poland, 40-653 Jagiellonian University Institute of Cardiology Krakow, Poland, 31-202 Poznan University of Medical Sciences II Clinic of Cardiology Poznan, Poland, 61-701 National Institute of Cardiology Warszawa, Poland, 04-628 收起 <<
NCT01861548 - Completed - Poland ... 展开 >> Nofer Institute of Occupational Medicine, Department of Environmental Epidemiology Lodz, Poland, 91-348 Department of Pediatrics and Allergy, Medical University of Lodz, N. Copernicus Hospital, Lodz, Poland Lodz, Poland, 93-513 收起 <<
NCT00620217 Coronary Artery Disease Phase 2 Completed - Poland ... 展开 >> Institute of Cardiology Warsaw, Poland, 04-628 收起 <<

Tripelennamine HCl 参考文献

[1]Manohar M, Goetz TE, Humphrey S, Depuy T. H1-receptor antagonist, tripelennamine, does not affect arterial hypoxemia in exercising Thoroughbreds. J Appl Physiol (1985). 2002 Apr;92(4):1515-23.

[2]Wasfi IA, Abdel Hadi AA, et al. Comparative disposition of tripelennamine in horses and camels after intravenous administration. J Vet Pharmacol Ther. 2000 Jun;23(3):145-52.

[3]Styczynski PB, Blackmon RC, Groopman JD, Kensler TW. The direct glucuronidation of 2-amino-1-methyl-6-phenylimidazo[4,5-b] pyridine (PhIP) by human and rabbit liver microsomes. Chem Res Toxicol. 1993 Nov-Dec;6(6):846-51

[4]Oliveto AH, Slifer BL, Dykstra LA. Tripelennamine fails to enhance the morphine-like stimulus effects of pentazocine. Pharmacol Biochem Behav. 1988 Feb;29(2):397-401

[5]Yeh SY. Potentiation of pentazocine antinociception by tripelennamine in the rat. J Pharmacol Exp Ther. 1985 Dec;235(3):683-9

[6]Vaupel DB. Tripelennamine interactions with the psychotomimetic sigma agonist N-allylnormetazocine. Pharmacol Biochem Behav. 1989 Jul;33(3):717-20

Tripelennamine HCl 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.43mL

0.69mL

0.34mL

17.13mL

3.43mL

1.71mL

34.27mL

6.85mL

3.43mL

Tripelennamine HCl 技术信息

CAS号154-69-8
分子式C16H22ClN3
分子量 291.82
别名 去敏灵;盐酸曲吡那敏;扑敏宁;盐酸吡甲胺;盐酸吡苯胺 ;Pyribenzamine HCl;Tripelennamine hydrochloride
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Inert atmosphere,Room temperature
溶解度

DMSO: 25 mg/mL(85.67 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 100 mg/mL(342.68 mM)，配合低频超声助溶
动物实验配方

Tags: Tripelennamine | 154-69-8 | H1-Receptor Antagonist | GPCR/G Protein | Neuronal Signaling | Immunology/Inflammation | Metabolic Enzyme/Protease | Histamine Receptor | Endogenous Metabolite | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Tripelennamine HCl 纯度/质量文件 | Tripelennamine HCl 亚型比较 | Tripelennamine HCl 生物活性 | Tripelennamine HCl 临床数据 | Tripelennamine HCl 参考文献 | Tripelennamine HCl 实验方案 | Tripelennamine HCl 技术信息

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